Design, synthesis and evaluation of some novel 3(2H)-pyridazinone-2-yl acetohydrazides as acetylcholinesterase and butyrylcholnesterase inhibitors
Tijen Önkol, Mehtap Gökçe, İlkay Orhan and Fatma Kaynak
Gazi University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, 06330 Ankara-Türkiye,
Gazi University, Faculty of Pharmacy, Department of Pharmacognosy, 06330 Ankara-Ttürkiye,
Gazi University, Faculty of Pharmacy, Department of Microbiology, 06330, Hipodrom-Ankara-Türkiye
Abstract: In this study eighteen new N’-[(4-Substituephenyl)sulfonyl]-2-[4-(Substituephenyl)-piperazine]-3(2H)-pyridazinone-2-yl acetohydrazide V derivatives were synthesized as acetylcholinesterase and butyrylcholinesterase inhibitors. The acetylcholinesterase (AChE) and butyrylcholinesterase (BChe) inhibitory activity of V derivatives was measured using Ellman’s method. Some of N’-[(substituted phenyl)sulfonyl]-2-(6-substituted-3(2H)-pyridazinone-2-yl)acetohydrazides V showed inhibitory activities close galantamine at 0.05 mM 0.1 mM and 0.2 mM concentrations . According to screening data, the analog of derivatives of V which possessed CF 3 on para position of phenylsulfonyl ring improved anti-AChE activity. Also antimicrobial activity of the synthesized compounds have been evaluated. In general V Derivatives showed weak antibacterial activity when compared reference compounds. Also all the compounds are less potent than fluconazole against yeast like fungi.
Keywords: 3(2H)-Pyridazinone; p-substituted sulfonylchloride acetohydrazides; acetylcholinesterase (AChE) inhibitor; butyrylcholinesterase (BChE) inhibitor. |